Dosing & Uses
Dosage Forms & Strength
ophthalmic emulsion
- 0.05% (Restasis; single-use or multidose vials)
ophthalmic solution
- 0.09% (Cequa; single-use vial)
Keratoconjunctivitis Sicca
Indicated to increase tear production associated with keratoconjunctivitis sicca (dry eye)
Instill 1 gtt BID in each eye ~12 hr apart
If using single-dose vial, discard immediately after using in both eyes
May be used concomitantly with artificial tears, allowing a 15-minute interval between products
Dosing Considerations
Restasis: Increased tear production was not seen in patients currently taking topical anti-inflammatory drugs or using punctal plugs
Orphan Indications
Cornal Melting
- For use in corneal melting syndromes of known or presumed immunologic etiopathogenesis, including Mooren's ulcer
- Orphan indication sponsor: Allergan, Inc; 2525 Dupont Drive, P.O. Box 19534; Irvine, CA 92623-9534
Prevention of Graft Rejection
- Treatment of patients at high risk of graft rejection following penetrating keratoplasty
- Orphan indication sponsor: Allergan, Inc; 2525 Dupont Drive, P.O. Box 19534; Irvine, CA 92623-9534
Keratoconjunctivitis
- Treatment of vernal keratoconjunctivitis
- Treatment of herpes simplex virus stromal keratitis
- Orphan indication sponsor: NOVAGALI Pharma SA; Batiment Genavenir IV F-91058-Evry cedex; France
Keratoconjunctivitis Sicca
- Treatment of severe keratoconjunctivitis sicca associated with Sjogren's syndrome
- Orphan indication sponsor: University Of Georgia; College Of Veterinary Medicine, Department of Small Animal Medicine; Athens, GA 30602
Corneal Graft Rejection
- Prevention of corneal graft rejection
- Orphan indication sponsor: NOVAGALI Pharma SA; Batiment Genavenir IV F-91058-Evry cedex; France
Dosage Forms & Strength
ophthalmic emulsion
- 0.05% (Restasis; single-use or multidose vials)
Keratoconjunctivitis Sicca
Restasis only
<16 years: Safety and efficacy not established
≥16 years
- Instill 1 gtt BID in each eye ~12 hr apart
- If using single-dose vial, discard immediately after using in both eyes
- May be used concomitantly with artificial tears, allowing a 15-minute interval between products
Dosing Considerations
Restasis: Increased tear production was not seen in patients currently taking topical anti-inflammatory drugs or using punctal plugs
Adverse Effects
>10%
Pain on instillation of drops (22%)
Ocular burning (17%)
1-10%
Conjunctival hyperemia (6%)
Frequency Not Defined
Conjunctival hyperemia
Discharge
Epiphora
Eye pain
Foreign body sensation
Pruritus
Postmarketing Reports
Hypersensitivity (including eye swelling, urticaria, rare cases of severe angioedema, face swelling, tongue swelling, pharyngeal edema and dyspnea)
Superficial injury of the eye (from the vial tip touching the eye during administration)
Warnings
Contraindications
Known or suspected hypersensitivity to any of the ingredients in the formulation
Cautions
Remove contact lenses prior to administration
Do not touch eyelids with vial tip to avoid contamination
Do not use with contact lenses; lenses may be reinserted 15 minutes following administration ophthalmic emulsion/solution
Patients with decreased tear production typically should not wear contact lenses
Pregnancy & Lactation
Pregnancy
Clinical administration of cyclosporine ophthalmic emulsion 0.05% is not detected systemically following topical ocular administration, and maternal use is not expected to result in fetal exposure to the drug
Oral administration of cyclosporine to pregnant rats or rabbits did not produce teratogenicity at clinically relevant doses
Lactation
Cyclosporine is known to appear in human milk following systemic administration, but presence in human milk following topical treatment has not been investigated; although blood concentrations are undetectable following topical administration of cyclosporine ophthalmic, caution should be exercised when cyclosporine ophthalmic multidose is administered to a nursing woman; the developmental and health benefits of breastfeeding should be considered along with the mother’s clinical need for cyclosporine ophthalmic multidose and potential adverse effects on the breast-fed child from cyclosporine
Pregnancy Categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk. C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done. D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk. X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist. NA: Information not available.Pharmacology
Mechanism of Action
Exact mechanism of action is not known
Calcineurin inhibitor; immunosuppressive agent when administered systemically
In patients whose tear production is presumed to be suppressed due to ocular inflammation associated with dry eyes, cyclosporine emulsion is thought to act as a partial immunomodulator
Absorption
Emulsion: There was no detectable drug accumulation in blood during 12 months of treatment
Solution: Blood concentrations of cyclosporine after twice daily topical ocular administration into each eye of healthy subjects for up to 7 days, and once on Day 8, were either not detectable or were marginally above the lower limit of assay quantitation of 0.1 ng/mL for up to 2 hr after a single dose, and up to 4 hr after multiple doses
Administration
Ophthalmic Administration
Single-use solution or emulsion: After opening for administration to one or both eyes use immediately, and discard remaining contents immediately
Do not administer while wearing contact lenses; remove contacts prior to administration; contacts may reinsert 15 minutes following administration
Storage
Emulsion: Store at 15-25°C (59-77°F)
Solution: Store at 20-25°C (68-77°F); store single-use vials in the original foil pouch
Images
Patient Handout
Formulary
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